萘酰亚胺-多胺缀合物的合成及体外抗癌活性

Synthesis and in vitro cytotoxicity of naphthalimide polyamine conjugates as antitumor agents

摘要:
合成了6个萘酰亚胺-多胺缀合物, 化合物的结构经元素分析、¹H NMR、¹³C NMR和MS确证。经MTT法对白血病细胞 (K562)、人乳腺癌细胞 (MB-231) 和前列腺癌细胞 (Ln cap cell) 进行了体外活性测试, 结果表明大多数化合物的体外抗肿瘤活性优于对照品氨萘非特 (amonafide), 其中化合物6d、6e和6f对正常人肝上皮细胞 (QSG-7701) 和肝癌细胞 (BEL-7402) 具有良好的选择性。

Abstract:
Six naphthalimide polyamine conjugates were synthesized and their structures were confirmed by elemental analysis, ¹H NMR, ¹³C NMR and MS. Antitumor activities were evaluated in vitro using MTT assay on Leukemia cells (K562), human breast cancer cells (MB-231) and prostate cancer cells (Ln cap cell). The results showed that most of the six compounds were superior to the control (amonafide), 6d, 6e, and 6f exhibited nice selectivity in a screen of hepatoma cells (BEL-7402) and human normal hepatocytes (QSG-7701).